Xiao Xiao, Wang Ting, Li Leijiao, Zhu Zhongli, Zhang Weina, Cui Guihua, Li Wenliang
School of Pharmacy, Jilin Medical University, Jilin, China.
Center for Biomaterials, Jilin Medical University, Jilin, China.
Front Pharmacol. 2019 Feb 19;10:110. doi: 10.3389/fphar.2019.00110. eCollection 2019.
A strategy for preparing composite micelles (CM) containing both cisplatin(IV) [CisPt(IV)] prodrug and capecitabine using a co-assembly method is described in this study. The CM are capable of an effective release of the anticancer drug cisplatin(II) [CisPt(II)] and capecitabine via acid hydrolysis once they are internalized by cancer cells. Moreover, the CM display a synergistic effect and the combination therapy in the micellar dosage form leads to reduced systemic toxicity and enhanced antitumor efficacy .
本研究描述了一种使用共组装方法制备同时包含顺铂(IV)[CisPt(IV)]前药和卡培他滨的复合胶束(CM)的策略。一旦被癌细胞内化,CM能够通过酸水解有效释放抗癌药物顺铂(II)[CisPt(II)]和卡培他滨。此外,CM显示出协同效应,胶束剂型的联合治疗导致全身毒性降低和抗肿瘤疗效增强。